Dietary supplements containing extracts of aronia and methods of using same to promote weight loss

ABSTRACT

A dietary supplement composition comprising aronia extract containing at least 20% anthocyanins by dry weight. The aronia extract is derived from the aronia melanocarpa plant. The aronia extract comprises approximately 10%-30% of the dry weight of the composition. A vitamin, weight loss agent, or antioxidant is provided in the composition. The dietary supplement composition is administered orally to promote weight loss.

CROSS-REFERENCE TO RELATED APPLICATION

This Application is a Divisional of U.S. Utility patent application Ser.No. 12/396,293, filed Mar. 2, 2009, entitled DIETARY SUPPLEMENTSCONTAINING EXTRACTS OF ARONIA AND METHODS OF USING SAME TO PROMOTEWEIGHT LOSS, the entirety of which is incorporated herein by reference.

STATEMENT REGARDING FEDERALLY SPONSORED RESEARCH OR DEVELOPMENT

n/a

FIELD OF THE INVENTION

The present invention relates to dietary supplement compositionscontaining aronia extracts and method for promoting weight loss.

BACKGROUND OF THE INVENTION

Obesity and Type II diabetes are quickly becoming an epidemic in theUnited States. The increased incidence of these conditions has beenattributed to diets characterized by high fat intake and repeatedingestion of refined foods and sugars, coupled with low fiber andvegetable intake. While obesity may be linked to lifestyle habits,obesity also impacts, and is impacted by, human physiology andneurology. A myriad of genetic, neurological, and other unknown factorsare also likely to play a role in the development of obesity. While twothirds of the world's population is defined as overweight, obesityrelated illnesses are rapidly becoming the leaders in the world's mostlethal diseases. For example, about 97 million adults in the UnitedStates are overweight, of which over 40 million are classified as obese.General obesity, known as adiposity, greatly increases the risk of manydiseases such as hypertension, type 2 diabetes, coronary heart disease,stroke, gallbladder disease, osteoarthritis, sleep apnea and otherrespiratory problems, and endometrial, breast, prostate, and coloncancers. Also, people with higher than normal body weights suffer from ahigher than normal early death rate. According to the NationalInstitutes of Health, each year about 280,000 adult deaths in the UnitedStates may be attributed, in part, to obesity. Many treatments for themanagement of weight and obesity and the maintenance of weight lossexist. In fact, approximately, 40 percent of women and 24 percent of menare trying to actively lose weight at any given time. These treatmentsare numerous and include all sorts of diets, increased physicalexercise, behavioral therapies, dietary supplementation,pharmacotherapy, hypnotherapy, surgery, or combinations of the above.

One such treatment involves the use of chemical compounds that inhibitabsorption of nutrients, such as fats or carbohydrates, as an approachto reducing caloric intake. Other compounds simply work to stimulatemetabolic rate through enhanced thermogenesis. However, the safety andefficacy of long-term administration of many weight loss compounds aresimply unknown. Moreover, history has shown that certain biologicalpathways, for example, stimulating thermogenesis with compounds likeephedra or Phen-Fen®, may not be the best approach.

An additional avenue to target obesity entails the use of supplementsand pharmaceuticals that target weight loss. These supplements andpharmaceuticals target appetite or satiety by using chemical messengerssuch as neuropeptides, CCK, Obestatin, Ghrelin, Enterostatin, Bombesin,CRF or many others. More recently the proliferator-activatedreceptor-gamma (PPARγ) system has evolved as a novel approach to weightloss and adipocyte differentiation. Other weight loss systems focus onregulating adipose hormones such as leptin, thyroid production, fattyacid synthase, or uncoupling certain proteins. The biological pathwaysinvolved in these regulation systems are complex and often redundant.Moreover, the body counteracts impacts on these regulation systems as itstrives for homeostasis. Therefore, what is needed is a dietarysupplement that is safe and effective at targeting weight loss.

One potential effective dietary supplement may be derived from thearonia fruit, which is one of the world's more obscure fruits. Aroniacontains a dense concentration of anthocyanins, which are aqueouspigments that may appear as a variety of colors including, red, purple,or blue. They belong to a parent class of molecules called flavonoids,which are known for their powerful antioxidant potential. Anthocyaninsoccur in all tissues of higher plants, including leaves, stems, roots,flowers, and fruits. The aronia plant, which grows in areas of high UVconcentrations, has developed defense mechanisms, such as phenolicanthocyanins, to help protect the plant from high UV radiation. As such,the aronia plant boasts one of the highest concentrations of antioxidantcapacity. Moreover, research has shown aronia extracts to be potentiallyeffective at reducing cardiovascular disease as well as improving musclerecovery. Aronia has also been shown to normalize the carbohydratemetabolism in diabetic rats as well as suppress the growth of certaincancer cells in rats. However, aronia's effects on adipose tissue arelargely unknown. Additionally, the concentrations of anthocyanins fromaronia that will promote weight less have previously been unknown. It istherefore desirable to provide a dietary supplement compositioncontaining an aronia extract to promote weight loss and fat managementas well as other health benefits.

SUMMARY OF THE INVENTION

It is to be understood that both the following summary and the detaileddescription are exemplary and explanatory and are intended to providefurther explanation of the invention as claimed. Neither the summary northe description that follows is intended to define or limit the scope ofthe invention to the particular features mentioned in the summary or inthe description

In accordance with an aspect, the present invention provides a dietarysupplement composition including extracts of aronia containing at least20% anthocyanins by dry weight.

In accordance with another aspect, the present invention provides adietary supplement composition including an aronia melanocarpa extractcontaining at least 20% anthocyanins by dry weight. The aroniamelanocarpa extract is approximately 10%-30% of the dry weight of thecomposition. At least one vitamin, weight loss agent, or antioxidant isalso included in the dietary supplement composition.

In accordance with yet another aspect, the present invention provides amethod for promoting weight loss. The method includes administeringcomposition comprising aronia melanocarpa extracts containing at least0.01% anthocyanins by dry weight, wherein the aronia melanocarpa extractis approximately 0.01%-99.9% if the dry weight of the composition.

BRIEF DESCRIPTION OF THE DRAWINGS

A more complete understanding of the present invention, and theattendant advantages and features thereof, will be more readilyunderstood by reference to the following detailed description whenconsidered in conjunction with the accompanying drawings wherein:

FIG. 1 is a flow chart of an exemplary method for promoting weight lossin rats in accordance with the principals of the present invention;

FIG. 2 is a table illustrating biological effects of the dietarysupplement composition of the present invention;

FIG. 3 is a chart illustrating effects of the dietary supplement of thepresent invention with respect to insulin signaling and mRNA expressionin the adipose, liver, and small intestine tissue;

FIG. 4 is a chart illustrating effects of the dietary supplement of thepresent invention with respect to CD36, fatty acid transporter andPPARγ, lipid sensor, and mRNA expression in adipose, liver, and smallintestine tissue;

FIG. 5 is a chart illustrating effects of the dietary supplement of thepresent invention with respect to mRNA expression related to lipidmetabolism in adipose, liver and small intestine tissue; and

FIG. 6 is a chart illustrating effects of the dietary supplement oninflammatory factor mRNA expression in adipose, liver and smallintestine tissue.

DETAILED DESCRIPTION OF THE INVENTION

The present invention advantageously provides for an aronia extractcomposition that promotes weight loss. The Aronia plant and berries maybe obtained from various parts of the world, including northern Europeand America. In an exemplary embodiment, an extract of aronia is derivedfrom the fruit of aronia melanocarpa, which may contain between0.01%-100% anthocyanins by dry weight. The aronia extract dietarysupplement may be in pharmaceutical dietary supplement compositions insolid, semi-solid, or liquid dosage forms, such as, for example,tablets, chewables, suppositories, pills, capsules, powders, liquids, orsuspensions, and may be provided in unit dosages suitable for a singleadministration. Time release preparations are also contemplated aseffective dosage formulations. The compositions may include an effectiveamount of a selected substrate in combination with a pharmaceuticallyacceptable carrier and, in addition, may include other medicinal agents,pharmaceutical agents, carriers, or diluents.

In a solid composition embodiment, conventional nontoxic solid carriersmay include, for example, pharmaceutical grades of mannitol, lactose,starch, magnesium stearate, sodium saccharine, talc, cellulose, glucose,sucrose and magnesium carbonate. Liquid pharmaceutically administrablecompositions may, for example, be prepared by dissolving or dispersingan active compound with optimal pharmaceutical adjuvants in anexcipient, such as water, saline, aqueous dextrose, glycerol, orethanol, to form a solution or suspension. For example, thepharmaceutical composition may contain minor amounts of nontoxicauxiliary substances such as wetting or emulsifying agents, pH bufferingagents, for example, sodium acetate or triethanolamine oleate. Actualmethods of preparing such dosage forms are known, or will be apparent,to those skilled in this art.

In an oral administration embodiment, fine powders or granules maycontain diluting, dispersing, or surface active agents. The fine powdersor granules may be presented in water or in syrup, in capsules orsachets in the dry state, or in a nonaqueous solution or suspension.Suspending agents may also be included in tablets, which may includebinders and lubricants in a suspension. Flavoring, preserving,suspending, thickening, or emulsifying agents may be also included tomodify the taste and texture of the composition. The tablets andgranules provided for oral administration may further be coated for easeof digestion.

In yet another embodiment, the aronia extract dietary supplementcomposition may be combined with one or more other components. Suchcomponents may include vitamins (such as vitamin A, vitamin B, vitaminC, vitamin D, or vitamin E), weight loss agents (such as synephrine,citrus aurantium, coleus, hoodia, hordenine, phenylethylamine, cinnamonextracts, evodiamine, sclareoliden, licorice oil, flavanoids,hydroxycitric acid, green tea, raspberry, guarana, yerba mate, ketone,white tea, oolong tea, fucoxanthin, or 7-keto dhea), antioxidants (suchas acai, wolfberry, alpha lipoic acid, astazanthin, or fucoxanthin), orany combination of the above. In an exemplary embodiment, the dietarysupplement may further include anthocyanins expressed in the form ofcyanadin-3-galactose, or salts, isomers, or derivatives ofcyanadin-3-galactose, which may further provide for increased weightloss.

It is further contemplated that variable dosing regiments are operativein the method of treatment. While in some instances, a single dosetreatment may be effective in producing therapeutic effects, in otherinstances a treatment period in the range of, for example, six weeks tothree months may be utilized. The composition may be administeredorally, parentally, or intravenously by intramuscular, intraperitoneal,or transdermally injection. Injectables may be prepared in conventionalforms, either liquid solutions or suspensions, solid forms suitable forsolution or prior to injection, or as suspension in liquid prior toinjection or as emulsions. The dose of the dietary supplementcomposition may vary depending on the age, weight, general condition ofthe user. For example, dosage is in the range of 1-1,000 mg ofequivalent of dry aronia powder extract per day may be an effectiverange. The aronia extract may also comprise 0.01%-100% of the dry weightof the composition. For example, an aronia dietary supplementcomposition may comprise 10%-30% of the dry weight of the composition.

The examples presented below are intended to illustrate a particularembodiment of the invention and are not intended to limit the scope ofthe specification, including the claims, in any way.

Example #1

Aronia melanocarpa 10% anthocyanins 200 mg Green Tea 45% egcg 300 mgCaffeine anhydrous 100 mg Evodiamine 100 mg 7-Keto DHEA 100 mg

Example #2

Aronia melanocarpa 25% anthocyanins 100 mg Green Tea 45% egcg 300 mgCinnulin PF 250 mg White Tea 100 mg Hoodia Gordonii 100 mg

Example #3

Aronia melanocarpa 25% anthocyanins 300 mg Green Tea 45% egcg 300 mgCinnulin PF 250 mg White Tea 100 mg Hoodia Gordonii 100 mg Acai Berry100 mg

Example #4

Aronia melanocarpa 25% anthocyanins 250 mg Green Tea 45% egcg 300 mgsynephrine  20 mg PEA  50 mg Hordenine 100 mg caffeine 200 mg yerba mate200 mg

Example #5

Aronia melanocarpa 15% anthocyanins 250 mg Hydroxycitric acid 500 mggreen coffee extract 150 mg fucoxanthin 200 mg white tea extract 200 mgguarana 500 mg

The efficacy and impacts of the aronia extracts on rats are illustratedbelow. The following abbreviations are used in the following paragraphs:CD36: Cluster of Differentiation 36; GYS: glycogen synthase; IL:interleukin; IR: insulin receptor; IRS-1: insulin receptor substrate-1;NPC1L1: Niemann-Pick C1 Like 1; PI3K: Phosphoinositide 3-kinase; PPAR:peroxisome proliferator-activated receptor; PTEN: phosphatase and tensinhomolog deleted on chromosome ten; SCARB1: Scavenger receptor class Btype I; SREBF1: sterol regulatory element binding transcription factor1; SREBP: sterol regulatory element binding protein; and TNF, tumornecrosis factor.

Initially, dry extracts of from the aronia plant are concentration andstandardized to contain 25% anthocyanins by dry weight, known ascellberry (“CB”), and tested on rats. As shown in FIG. 1, male rats werefed with a fructose diet four weeks. The rats were divided randomly intothree groups, each group having a similar mean body weights, with sixrats in each group. Control rats were fed a standard diet four weeks,and other two groups of rats were given either 100 mg or 200 mg/kg ofbodyweight per day of an aronia extract containing 25% anthocyanins inthe rats' drinking water. The body weight and food intake were evaluatedfor three-days each week, and the diet intake of each CB administeredgroup during the experimental period was similar to that of the controlgroup.

Now Referring to FIG. 2, after consuming the CB composition for fourweeks, the body weights of two experimental groups were significantlyreduced compared to the control group. Also, there was minimalstatistical difference in bodyweight amongst the experimental groupstreated with the CB composition. Both doses of the CB compositionadministered to the rats inhibited epididymal adipose tissue weight,compared with the control group. Additionally, the experimental groupstreated with the CB compositions showed an improved blood glucoselevels, as well decreased triglyceride, cholesterol, free fatty acids,and LDL-C concentrations. The experimental rat groups treated with CBalso showed improved serum insulin and HDL-C levels. The data suggeststhat the administered CB composition improves the lipid disorders foundin fructose-fed insulin resistant rats.

Now referring to FIG. 3, insulin signaling is known to affect hepaticglucose production and glucose uptake in muscle and adipose tissue, aswell as influence the fat deposition in adipose tissue, hepatic andintestinal lipid metabolism. Disruption of insulin signaling can affectkey cellular pathways that serve to maintain energy balance and glucosehomeostasis, which can then lead to insulin resistance and progressiontoward various metabolic disorders, including cardiovascular disease,obesity, and type 2 diabetes. High-fructose diets often induce systemicand peripheral insulin resistance.

As shown in FIG. 3, however, consumption of the CB composition improvesthe mRNA expression of insulin signaling in adipose, liver and smallintestine tissue. The administered CB composition increased mRNAexpression of insulin receptor (35%), IRS1 (130%), IRS2 (80%), PI3Kr1(158%), Akt1 (10%) in the adipose tissue compared with the controlgroup. The CB treated rats also showed increased mRNA changes in theadipose tissue GLUT4, a major glucose transporter in muscle and adiposecells. The mRNA level of PTEN, a tumor suppressor, which negativelyregulates insulin signaling, was also reduced significantly.

Continuing to refer to FIG. 3, consumption of the CB composition by theexperimental rat group exhibit improved mRNA expression in the liver ofinsulin receptor (8%), IRS1 (18%), IRS2 (36%), Akt1 (19%), PI3Kr1 (13%)and decreases the expression of PTEN (65%), compared with the controlgroup. The administered CB composition also improves the mRNA expressionin the small intestine of IR (33%), IRS1 (47%), IRS2 (24%), Akt1 (15%),P13Kr1(140%) and decreased the expression of PTEN (27%) compared withthe control group. The data suggest that CB consumption improves themRNA expression of insulin signaling in adipose, liver, and smallintestine tissue leading to improved glucose and lipid metabolism.

Now referring to FIG. 4, CD36, a fatty acid translocase, is acell-surface glycoprotein that functions as a multi-ligand receptor ortransporter involved in various diverse physiological processes anddisorders, including atherosclerosis, dyslipidemia, insulin resistanceand diabetes. Defective function or expression of CD36 may result indyslipidemia or insulin resistance. Moreover, an increased expression ofhepatic CD36 protein in response to diet-induced obesity may exacerbatehepatic triglyceride storage and secretion. As shown in FIG. 4, the CBtreated rats exhibit decreased expression of CD36 (57%) in the livertissue, which may improve overall lipid metabolism.

Continuing to refer to FIG. 4, CD36 may also be important forchylomicron production and acute fatty acid uptake in the smallintestine. In the small intestine tissue of CB administered rats, anincrease in the mRNA expression of CD36 (140%) was observed. This resultsuggests that the CB composition may regulate lipid absorption andtransfer.

PPARγ is expressed in high levels in adipose tissue and plays a role inincreasing insulin sensitivity as well as in promoting fatty acid uptakeinto adipocytes and adipocyte differentiation. The net effect of theseprocesses is to increase triglyceride storage in adipocytes, reducingdelivery of fatty acids to the liver. As shown in FIG. 4, the CBadministered rats exhibit an increased PPARγ expression in adipose andliver tissue of the CB treated rats. The CB administered rats alsoexhibit and increased mRNA expression of PPARγ (170%) in the smallintestine tissue. The data suggests that the CB composition enhancesPPARγ expression, which improve insulin sensitivity, thereby regulatinglipid metabolism in these tissues.

Now referring to FIG. 5, sterol regulatory element binding protein(SREBP)1c is a master regulator of lipogenic gene expression in adiposeand liver tissue. The expressions of adipogenesis-related genes,including SREBP1c, may decrease in the adipose of animal tissue exposedto a long term high fat diet. As shown in FIG. 5, the CB administeredrats exhibit enhanced mRNA expression of SREBP1c (35%) in the adiposetissue compared with the control group. The CB administered rats alsoexhibit enhanced mRNA expression of sterol regulatory element bindingtranscription factor 1 (SREBF1) (47%), which may play an important rolein regulation of adipose fat deposition. Moreover, the CB administeredrats exhibit increased adipose (51%) and hepatic (72%) glycogensynthase.

Continuing to refer to FIG. 5, SREBP1c also has a crucial role in theregulation of triglyceride accumulation in the liver and theoverproduction of intestinal derived apoB48. An increase of SREBF1 maybe associated with greater concentrations of triglycerides. The CBadministered rats exhibit decreased mRNA expression of SREBP1c (44%) andSREBF1 (48%) in the liver as well as SREBF1 (32%) in the small intestinetissue.

Scavenger receptor class B type I (SCARB1) is expressed in enterocytebrush border membranes mainly at the top of intestinal villosities andin the proximal part of intestine where cholesterol absorption mainlyoccurs. Over expression of SCARB1 in the small intestine may increaseintestinal absorption of both cholesterol and triglycerides. As shown inFIG. 5, the CB administered rats exhibit decreased mRNA expression ofSCARB1 (27%) in the small intestine tissue.

Niemann-Pick C1 Like 1 (NPC1L1) is a protein localized in jejunalenterocytes that is critical for small intestinal cholesterolabsorption. Inactivation of NPC1L1 may cause multiple lipid transportdefects and protects against diet-induced hypercholesterolemia. The CBadministered rats exhibit significantly enhanced NPC1L1 expression inthe small intestine. In contrast to the intestinal tissue, the CBadministered rats exhibit a decreased NPC1L1 expression in liver tissue.The data from the adipose, liver, and small intestinal tissue show thatCB consumption may be useful to regulate gene expression related toadipogenesis, hepatic, and small intestinal lipid metabolism.

Now referring to FIG. 6, obesity and inflammation are highly integratedprocesses in the pathogenesis of insulin resistance, diabetes, andatherosclerosis. Obesity may induce a pro-inflammatory state, which maycause or worsen insulin resistance in adipose tissue, liver, and thesmall intestine. In abdominal obesity, the high mass of visceral adiposetissue may be extremely active metabolically and secrete manyinflammatory cytokines and chemokines having effects at local andsystemic level. Insulin resistance is associated with a state of chroniclow-grade inflammation. Several mediators released from various celltypes, including immune cells and adipocytes, have been identified asbeing involved in the development of insulin resistance. Among those areseveral pro-inflammatory cytokines such as tumor necrosis factor(TNF)-α, interleukin (IL)-1β, IL-6, and various adipocytokines. Theinflammatory factor TNF-α may induce systemic, small intestinal, andhepatic insulin resistance, as well as stimulate apoB48 and systemicdyslipidemia.

As shown in FIG. 6, the CB administered rats exhibit decreased mRNAexpression of IL-1β (51%), TNF-α (25%), and IL-6 (42%) in the adiposetissue. The CB administered rats also exhibit decreased mRNA expressionof IL-1β (47%), TNF-α (46%), IL-6 (39%) in the liver, as well asdecreased mRNA expression of IL-1β (53%), TNF-α (55%), IL-6 (58%) in thesmall intestine tissue, compared with the control group.

These results demonstrate that CB consumption may improve blood glucose,serum lipid profiles, adipose tissue mass and bodyweight gain byregulating the multiple genes in adipogenesis, glucose, lipid andinflammatory pathways. CB consumption may also be beneficial in humansfor managing metabolic syndrome including obesity, dyslipidemia andinsulin resistance.

It will be appreciated by persons skilled in the art that the presentinvention is not limited to what has been particularly shown anddescribed herein above. In addition, unless mention was made above tothe contrary, it should be noted that all of the accompanying drawingsare not to scale. A variety of modifications and variations are possiblein light of the above teachings without departing from the scope andspirit of the invention, which is limited only by the following claims.

1. (canceled)
 2. (canceled)
 3. A method of promoting weight loss in ahuman comprising: administering a dosage of a composition comprising anaronia melanocarpa extract, the aronia melanocarpa extract containing atleast 10% anthocyanins by dry weight, and wherein the dosage of thearonia melanocarpa extract is provided in a range from about 50 mg toabout 400 mg per dosage unit.
 4. The method of claim 3, wherein thedosage unit is provided in a range from about 400 mg to about 1,200 mg.5. The method of claim 3, wherein the composition is administered inpowdered form.
 6. The method of claim 3, wherein the composition isadministered in tablet form.
 7. The method of claim 3, wherein thecomposition is administered in liquid form as a suspension.
 8. Themethod of claim 3, wherein the anthocyanins includecyanadin-3-galactose.
 9. The method of claim 3, wherein the compositionis administered at least once a day.
 10. A method of promoting weightloss in a human comprising: administering a dosage of a compositioncomprising an aronia melanocarpa extract, the aronia melanocarpa extractcontaining at least 10% anthocyanins by dry weight; the compositionfurther including green tea.
 11. The method of claim 10, wherein thegreen tea is provided in a range from about 200 mg to about 300 mg perdosage unit.
 12. The method of claim 11, where the green tea contains atleast 25% epigallocatechin gallate (egcg) by dry weight.
 13. The methodof claim 10, wherein the dosage unit is provided in a range from about400 mg to about 1,200 mg.
 14. The method of claim 10, wherein the aroniamelanocarpa extract is provided in a range from about 50 mg to about 400mg per dosage unit.
 15. The method of claim 10, wherein the compositionis administered at least once a day.
 16. The method of claim 10, whereinthe composition is administered in powdered form.
 17. The method ofclaim 10, wherein the composition is administered in liquid form as asuspension.
 18. The method of claim 13, wherein the composition furtherincludes cinnamon.
 19. The method of claim 13, wherein the compositionfurther includes raspberry ketone.
 20. The method of claim 13, whereinthe composition further includes citrus aurantium.
 21. The method ofclaim 13, wherein the composition further includes white tea.
 22. Amethod of promoting weight loss in a human comprising: administering atleast once a day a dosage or a tablet of a capsule compositioncomprising an aronia melanocarpa extract provided in a range from about50 mg to about 400 mg per dosage unit; the aronia melanocarpa extractcontaining at least 10% anthocyanins by dry weight, wherein theanthocyanins include cyanadin-3-galactose; the composition furtherincluding green tea containing at least 25% epigallocatechin gallate(egcg) by dry weight, wherein the green tea is provided in a range fromabout 200 mg to about 300 mg per dosage unit; the composition furtherincluding raspberry ketone and citrus aurantium; and wherein the dosageunit is provided in a range from about 400 mg to about 1,200 mg.